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ENOXAPARIN
Lakshmi Narayana M
■ Introduction
■ Mechanism of action
■ Pharmacokinetics
■ Indications
■ Recommended dosing schedule
■ Contraindications/ Precautions
■ Possible side effects
Areas to cover….
Introduction
■ It is an anticoagulant medication (blood thinner).
■ Enoxaparin belongs to the class of drugs known as low molecular weight heparins
(LMWH).
■ Enoxaparin was first made in 1981 and approved for medical use in 1993.
■ It is on theWorld Health Organization's List of Essential Medicines, the most effective
and safe medicines needed in a health system.
■ Enoxaparin is made from heparin.
Mechanism of action…
■ Enoxaparin binds to and accelerates the activity of antithrombin III. By activating
antithrombin III, enoxaparin preferentially potentiates the inhibition of coagulation
factors Xa and IIa. Factor Xa catalyses the conversion of prothrombin to thrombin, so
enoxaparin's inhibition of this process results in decreased thrombin and ultimately
the prevention of fibrin clot formation. Low molecular weight heparins are less
effective at inactivating factor IIa due to their shorter length.
Pharmacokinetics
 Absorption:
Mean absolute bioavailability of enoxaparin, after 1.5 mg/kg given subcutaneously is
100 %.
 Distribution:
80% bound-albumin
 Metabolism:
Undergoes desulfation and polymerization via the liver, half life is 4.5 hr
 Elimination:
Renal clearance of active fragments represents about 10% of the administered dose
and total renal excretion of active and non-active fragments 40% of the dose.
Indications
■ Treatment of unstable angina (UA) and non-Q-wave myocardial infarction (NQMI),
administered concurrently with aspirin
■ DVT prophylaxis in knee replacement surgery
■ DVT prophylaxis in hip replacement surgery
■ DVT prophylaxis in abdominal surgery
■ Treatment of DVT with or without pulmonary embolism
■ Treatment of DVT inpatient, with ST-segment elevation myocardial infarction (STEMI)
Note: DVT: Deep vain thrombosis (formation of blood clots.)
Recommended dosing schedule
■ UsualAdult Dose
1 to 1.5 mg/kg sc for every 12 hrs
■ Acute ST segment elevation myocardial infarction:
A single 30 mg intravenous bolus plus a 1 mg/kg subcutaneous dose followed by
1 mg/kg subcutaneously every 12 hours
■ Usual Pediatric Dose
less than 2 months: 1.5 mg/kg subcutaneously every 12 hours.
2 months to 17 years: 1 mg/kg subcutaneously every 12 hours.
Contraindications/Precautions
■ Enoxaparin is contraindicated in patients with active major bleeding, thrombocytopenia,
and patients with hypersensitivity to benzyl alcohol and/or pork products.
■ Use with caution in patients with a history of heparin-induced thrombocytopenia and those
at an increased risk of bleeding.Therapy should be discontinued in the event of severe
haemorrhage
■ Enoxaparin is intended for subcutaneous and intravenous administration. It should not be
administered by intramuscular injection.
Possible side effects
■ Local reactions: local irritation, pain, hematoma, ecchymosis, erythema
■ Bleeding
■ Hyperkalemia
■ Transaminitis
■ Hemorrhage
Box warning in next slide!!!!
Enoxaparin
Enoxaparin

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Enoxaparin

  • 2. ■ Introduction ■ Mechanism of action ■ Pharmacokinetics ■ Indications ■ Recommended dosing schedule ■ Contraindications/ Precautions ■ Possible side effects Areas to cover….
  • 3. Introduction ■ It is an anticoagulant medication (blood thinner). ■ Enoxaparin belongs to the class of drugs known as low molecular weight heparins (LMWH). ■ Enoxaparin was first made in 1981 and approved for medical use in 1993. ■ It is on theWorld Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system. ■ Enoxaparin is made from heparin.
  • 4. Mechanism of action… ■ Enoxaparin binds to and accelerates the activity of antithrombin III. By activating antithrombin III, enoxaparin preferentially potentiates the inhibition of coagulation factors Xa and IIa. Factor Xa catalyses the conversion of prothrombin to thrombin, so enoxaparin's inhibition of this process results in decreased thrombin and ultimately the prevention of fibrin clot formation. Low molecular weight heparins are less effective at inactivating factor IIa due to their shorter length.
  • 5. Pharmacokinetics  Absorption: Mean absolute bioavailability of enoxaparin, after 1.5 mg/kg given subcutaneously is 100 %.  Distribution: 80% bound-albumin  Metabolism: Undergoes desulfation and polymerization via the liver, half life is 4.5 hr  Elimination: Renal clearance of active fragments represents about 10% of the administered dose and total renal excretion of active and non-active fragments 40% of the dose.
  • 6. Indications ■ Treatment of unstable angina (UA) and non-Q-wave myocardial infarction (NQMI), administered concurrently with aspirin ■ DVT prophylaxis in knee replacement surgery ■ DVT prophylaxis in hip replacement surgery ■ DVT prophylaxis in abdominal surgery ■ Treatment of DVT with or without pulmonary embolism ■ Treatment of DVT inpatient, with ST-segment elevation myocardial infarction (STEMI) Note: DVT: Deep vain thrombosis (formation of blood clots.)
  • 7. Recommended dosing schedule ■ UsualAdult Dose 1 to 1.5 mg/kg sc for every 12 hrs ■ Acute ST segment elevation myocardial infarction: A single 30 mg intravenous bolus plus a 1 mg/kg subcutaneous dose followed by 1 mg/kg subcutaneously every 12 hours ■ Usual Pediatric Dose less than 2 months: 1.5 mg/kg subcutaneously every 12 hours. 2 months to 17 years: 1 mg/kg subcutaneously every 12 hours.
  • 8. Contraindications/Precautions ■ Enoxaparin is contraindicated in patients with active major bleeding, thrombocytopenia, and patients with hypersensitivity to benzyl alcohol and/or pork products. ■ Use with caution in patients with a history of heparin-induced thrombocytopenia and those at an increased risk of bleeding.Therapy should be discontinued in the event of severe haemorrhage ■ Enoxaparin is intended for subcutaneous and intravenous administration. It should not be administered by intramuscular injection.
  • 9. Possible side effects ■ Local reactions: local irritation, pain, hematoma, ecchymosis, erythema ■ Bleeding ■ Hyperkalemia ■ Transaminitis ■ Hemorrhage Box warning in next slide!!!!